Tyrosyl-DNA Phosphodiesterases 1 and 2 (Tdp1 and Tdp2) can repair damaged DNA resulting from topoisomerase inhibitors (e.g. Top1) and a variety of other DNA-damaging agents. 7-Azaindenoisoquinolines that are inhibitors of each of Top1, Tdp1 and Tdp2 are disclosed. Also described are methods for preparing azaindenoisoquinoline and methods for treating patients of a cancer using the disclosed azaindenoisoquinoline compounds or a pharmaceutical formulation thereof.
酪
氨酰-DNA
磷酸二酯酶 1 和 2(Tdp1 和 Tdp2)可以修复拓扑异构酶
抑制剂(如 Top1)和其他多种 DNA 损伤剂造成的受损 DNA。7-Azaindenoisoquinolines 是 Top1、Tdp1 和 Tdp2 的
抑制剂。还描述了制备偶氮亚
氨基
异喹啉的方法和使用所公开的偶氮亚
氨基
异喹啉化合物或其药物制剂治疗癌症患者的方法。